Preclinical Characterization of the Selective JAK1 Inhibitor LW402 for Treatment of Rheumatoid Arthritis

References

• Smolen JS, Aletaha D. Rheumatoid arthritis therapy reappraisal: strategies, opportunities and challenges. Nat Rev Rheumatol. 2015;11:276–289. doi:10.1038/nrrheum.2015.8
   PubMed Web of Science ®Google Scholar
• Taylor PC, Moore A, Vasilescu R, et al. A structued literature review of the burden of illness and unmet needs in patients with rheumatoid arthritis: a current perspective. Rheumatol Int. 2016;36:685–695. doi:10.1007/s00296-015-3415-x
   PubMed Web of Science ®Google Scholar
• Morris R, Kershaw NJ, Babon JJ. The molecular details of cytokine signalling via the JAK/STAT pathway. Protein Sci. 2018;27:1984–2009.
   PubMed Web of Science ®Google Scholar
• O’Sullivan LA, Liongue C, Lewis RS, Stephenson SE, Ward AC. Cytokine receptor signaling through the Jak-Stat-Socs pathway in disease. Mol Immunol. 2007;44:2497–2506. doi:10.1016/j.molimm.2006.11.025
   PubMed Web of Science ®Google Scholar
• Vainchenker W, Dusa A, Constantinescu SN. JAKs in pathology: role of Janus kinases in hematopoietic malignancies and immunodeficiencies. Semin Cell Dev Biol. 2008;19:385–393. doi:10.1016/j.semcdb.2008.07.002
   PubMed Web of Science ®Google Scholar
• Michalska A, Blaszczyk K, Wesoly J, Bluyssen HR. A positive feedback amplifier circuit that regulates interferon (IFN)-stimulated gene expression and controls type I and type II IFN responses. Front Immunol. 2018;9:1135. doi:10.3389/fimmu.2018.01135
   PubMed Web of Science ®Google Scholar
• Ghoreschi K, Laurence A, O’Shea JJ. Janus kinases in immune cell signaling. Immunol Rev. 2009;228:273–287. doi:10.1111/j.1600-065X.2008.00754.x
   PubMed Web of Science ®Google Scholar
• O’Shea JJ, Pesu M, Borie DC, Changelian PS. A new modality for immunosuppression: targeting the JAK/STAT pathway. Nat Rev Drug Discov. 2004;3:555–564. doi:10.1038/nrd1441
   PubMed Web of Science ®Google Scholar
• O’Shea JJ, Plenge R. JAK and STAT signaling molecules in immunoregulation and immune-mediated disease. Immunity. 2012;36:542–550. doi:10.1016/j.immuni.2012.03.014
   PubMed Web of Science ®Google Scholar
• Fridman JS, Scherle PA, Collins R, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010;184:5298–5307. doi:10.4049/jimmunol.0902819
   PubMed Web of Science ®Google Scholar
• Meyer DM, Jesson MI, Li X, et al. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis. J Inflamm. 2010;7:41. doi:10.1186/1476-9255-7-41
   Google Scholar
• Fleischmann R, Kremer J, Cush J, et al. Placebo-controlled trial of tofacitinib monotherapy in rheumatoid arthritis. New Engl J Med. 2012;367:495–507. doi:10.1056/NEJMoa1109071
   PubMed Web of Science ®Google Scholar
• Van Vollenhoven R, Takeuchi T, Pangan AL, et al. A phase 3, randomized, controlled trial comparing upadacitinib monotherapy to MTX monotherapy in MTX-naive patients with active rheumatoid arthritis. Arthritis Rheumatol. 2018;70:990–992.
   Google Scholar
• Milici AJ, Kudlacz EM, Audoly L, Zwillich S, Changelian P. Cartilage preservation by inhibition of Janus kinase 3 in two rodent models of rheumatoid arthritis. Arthritis Res Ther. 2008;10:R14. doi:10.1186/ar2365
   PubMed Web of Science ®Google Scholar
• Kudlacz E, Conklyn M, Andresen C, Whitney-Pickett C, Changelian P. The JAK-3 inhibitor CP-690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia. Eur J Pharmacol. 2008;582:154–161. doi:10.1016/j.ejphar.2007.12.024
   PubMed Web of Science ®Google Scholar
• Changelian PS, Flanagan ME, Ball DJ, et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003;302:875–878. doi:10.1126/science.1087061
   PubMed Web of Science ®Google Scholar
• Dowty ME, Jesson MI, Ghosh S, et al. Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis. J Pharmacol Exp Ther. 2014;348:165–173. doi:10.1124/jpet.113.209304
   PubMed Web of Science ®Google Scholar
• Cox L, Cools J. JAK3 specific kinase inhibitors: when specificity is not enough. Chem Biol. 2011;18:277–278. doi:10.1016/j.chembiol.2011.03.002
   PubMedGoogle Scholar
• Haan C, Rolvering C, Raulf F, et al. Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors. Chem Biol. 2011;18:314–323. doi:10.1016/j.chembiol.2011.01.012
   PubMed Web of Science ®Google Scholar
• Thoma G, Nuninger F, Falchetto R, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. J Med Chem. 2011;54:284–288. doi:10.1021/jm101157q
   PubMed Web of Science ®Google Scholar
• Wang Z, Fan GQ, Yang S, Zeng ZH Preparation of 1H-pyrrolo[2,3-d] pyrimidine derivatives as Jak kinase inhibitors. 2019. US-2019-0382408-A1.
   Google Scholar
• Brand DD, Latham KA, Rosloniec EF. Collagen-induced arthritis. Nat Protoc. 2007;2:1269–1275. doi:10.1038/nprot.2007.173
   PubMed Web of Science ®Google Scholar
• Lin HS, Hu CY, Chan HY, et al. Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents. Br J Pharmacol. 2007;150:862–872. doi:10.1038/sj.bjp.0707165
   PubMed Web of Science ®Google Scholar
• Ghoreschi K, Jesson MI, Li X, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). J Immunol. 2011;186:4234–4243. doi:10.4049/jimmunol.1003668
   PubMed Web of Science ®Google Scholar
• van Rompaey L, Galien R, van der Aar EM, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013;191:3568–3577. doi:10.4049/jimmunol.1201348
   PubMed Web of Science ®Google Scholar
• Williams NK, Bamert RS, Lucet IS. Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains. J Mol Biol. 2009;387:219–232. doi:10.1016/j.jmb.2009.01.041
   PubMed Web of Science ®Google Scholar
• Lee YH, Song GG. Comparison of the efficacy and safety of tofacitinib and filgotinib in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials. Z Rheumatol. 2019;79:590–603. doi:10.1007/s00393-019-00733-x
   Web of Science ®Google Scholar
• Greenwald MW, Fidelus-Grot R, Levy R, Liang J, Vaddi K, Williams WV. A randomized dose-ranging, placebo-controlled study of INCB028050, a selective JAK1 and JAK2 inhibitor in subjects with active rheumatoid arthritis. Arthritis Rheum. 2010;62:S911.
   PubMedGoogle Scholar
• O’Shea JJ, Holland SM, Staudt LM. JAKs and STATs in immunity, immunodeficiency, and cancer. N Engl J Med. 2013;368:161–170. doi:10.1056/NEJMra1202117
   PubMed Web of Science ®Google Scholar
• Kremer JM, Bloom BJ, Breedveld FC, Zwillich SH. The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo. Arthritis Rheum. 2009;60:1895–1905. doi:10.1002/art.24567
   PubMed Web of Science ®Google Scholar
• Fleischmann R, Pangan AL, Song I, et al. Upadacitinib versus placebo or adalimumab in patients with rheumatoid arthritis and an inadequate response to methotrexate: results of a phase 3, double‐blind, randomized controlled trial. Arthritis Rheumatol. 2019;71:1788–1800. doi:10.1002/art.41032
   PubMed Web of Science ®Google Scholar
• Parmentier JM, Voss J, Graff C, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018;2:23. doi:10.1186/s41927-018-0031-x
   PubMedGoogle Scholar
• Lee YH, Song GG. Comparative efficacy and safety of tofacitinib, baricitinib, upadacitinib, filgotinib and peficitinib as monotherapy for active rheumatoid arthritis. J Clin Pharm Ther. 2020;45:674–681. doi:10.1111/jcpt.13142
   PubMed Web of Science ®Google Scholar